Global Patent Index - EP 1078634 A1

EP 1078634 A1 2001-02-28 - Medicament for inhibiting NF-kB

Title (en)

Medicament for inhibiting NF-kB

Title (de)

Arzneimittel zur Hemmung von NF-kB

Title (fr)

Médicament pour inhiber le NF-kB

Publication

EP 1078634 A1 (DE)

Application

EP 99810750 A

Priority

EP 99810750 A

Abstract (en)

Indolo(2,1-b)quinazoline-6,12-diones of formula (I), salts of these and mixtures containing them, are used to inhibit the transcription factor NF- SIMILAR kB, to inhibit the enzyme cyclooxygenase, or to inhibit release of histamine and/or serotonin. Independent claims are included for: (A) use of indolo(2,1-b)quinazoline-6,12-dione of formula (I), salts of (I) or mixtures which contain at least one compound of formula (I), for: (i) preparation of medicaments for inhibiting the transcription factor NF- SIMILAR kB and/or for inhibiting cyclooxygenase ( COX) (preferably COX-2); (ii) preparation of medicaments with antiphlogistic (especially antirheumatic) activity for treatment of inflammatory disorders (especially rheumatoid disorders and arthritis); (iii) for preparation of medicaments for prevention, or assisting prevention, of Alzheimer's disease or cancer, or (iv) for preparation of long-term medicaments for prevention, or assisting prevention, of age-related disorders. (B) use of a mixture, which includes a plant extract which contains the active agent tryptanthrin (I; R<1>-R<8> = H), in preparation of medicaments for inhibiting the transcription factor NF- SIMILAR kB, for inhibiting COX (especially COX-2) and/or for inhibiting release of histamine and/or serotonin. (C) treatment of disorders by inhibiting the transcription factor NF- SIMILAR KB, by inhibiting COX-2 and/or by inhibiting release of histamine and/or serotonin, comprising use of a compound, salt or mixture as described in (A). R<1>-R<8> = H or some other substituent

Abstract (de)

Indolo[2,1-b]chinazolin-6,12-dione der Formel (1) <IMAGE> in der R1 bis R8 unabhängig voneinander gewählt sind aus Wasserstoffatomen und pharmazeutisch akzeptablen Substituenten, und pharmazeutisch akzeptable Salze von Verbindungen der Formel (1) zur Verwendung für Arzneimittel zur Hemmung des Trans-kriptionsfaktors NF-kB und/oder zur Hemmung von COX mit einer präferentiellen Hemmwirkung auf COX-2; solche Arzneimittel eigenen sich zur Verwendung als antiphlogistische, insbesondere antirheumatische Mittel zur Behandlung von entzündlichen Erkrankungen, insbesondere des rheumatischen Formenkreises und der Arthritiden, sowie zur präventiven oder adjuvanten Behandlung von Krebs und morbus Alzheimer sowie für die präventive oder adjunktive Dauermedikation gegen Altersbeschwerden.

IPC 1-7 (main, further and additional classification)

A61K 31/519; A61P 29/00; A61P 25/28; A61P 35/00; A61P 43/00

IPC 8 full level (invention and additional information)

A61K 31/519 (2006.01); A61P 25/28 (2006.01); A61P 29/00 (2006.01); A61P 35/00 (2006.01); A61P 43/00 (2006.01)

CPC (invention and additional information)

A61K 31/519 (2013.01)

Citation (search report)

  • [E] EP 0987027 A1 20000322 - HAYASHIBARA BIOCHEM LAB [JP]
  • [DX] WO 9513807 A1 19950526 - PATHOGENESIS CORP [US], et al
  • [X] KIMOTO T ET AL: "CYTOTOXIC EFFECTS OF SUBSTANCES IN INDIGO PLANT (POLYGONUM TINCTORIUM LOUR.) ON MALIGNANT TUMOR CELLS", NATURAL MEDICINES (SHOYAKUGAKU ZASSHI),JP,JAPANESE SOCIETY OF PHARMACOGNOSY, TOKYO, vol. 53, no. 2, April 1999 (1999-04-01), pages 72 - 79, XP000872614, ISSN: 1340-3443
  • [X] ZOU J C ET AL: "Minor constituents of qing dai, a traditional Chinese medicine. I. Isolation, structural determination and synthesis of tryptanthrin and qingdainone.", YAO HSUEH HSUEH PAO [ACTA PHARMACEUTICA SINICA], (1985 JAN) 20 (1) 45-51., XP000904795
  • [X] DATABASE WPI Section Ch Week 198020, Derwent Publications Ltd., London, GB; Class B02, AN 1980-35669C, XP002135731
  • [X] MITSCHER L A ET AL: "TUBERCULOSIS: A SEARCH FOR NOVEL THERAPY STARTING WITH NATURAL PRODUCTS", MEDICINAL RESEARCH REVIEWS,US,NEW YORK, NY, vol. 18, no. 6, November 1998 (1998-11-01), pages 363 - 374, XP000872677, ISSN: 0198-6325
  • [X] MITSCHER, LESTER A. ET AL: "Antimicrobial agents from higher plants. New synthesis and bioactivity of tryptanthrin (indol[2,1-b]quinazoline-6,12-dione) and its analogs", HETEROCYCLES ( 1981 ), 15(2), 1017-21, XP000904722
  • [X] GRANDOLINI G ET AL: "Synthesis and antimicrobial activity of some new derivatives of 6,12- dihydroindolo [2,1-b]quinazolin-6,12- dione.", FARMACO, (1997 NOV) 52 (11) 679-83., XP000891903
  • [X] HONDA G ET AL: "ISOLATION OF AN ANTIDERMATOPHYTIC, TRYPTANTHRIN, FROM INDIGO PLANTS, POLYGONUM TINCTORIUM AND ISATIS TINCTORIA", PLANTA MEDICA,DE,THIEME, STUTTGART, vol. 38, 1980, pages 275 - 276, XP000872217, ISSN: 0032-0943
  • [A] PATENT ABSTRACTS OF JAPAN vol. 007, no. 167 (C - 177) 22 July 1983 (1983-07-22)
  • [A] DATABASE WPI Section Ch Week 197817, Derwent Publications Ltd., London, GB; Class B04, AN 1978-31415A, XP002135732

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

EP 1078634 A1 20010228

INPADOC legal status


2002-05-29 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20010829

2001-11-14 [AKX] PAYMENT OF DESIGNATION FEES

- Free text: AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2001-02-28 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2001-02-28 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free text: AL;LT;LV;MK;RO;SI